R&D(research and development)

F573

Drug description

Purpose of use

F573 is a proprietary di-peptide small molecule compound with potent inhibitory effect on caspases, a class of enzymes critical for cell death and inflammatory response. Promising efficacy has also been shown in animal studies for liver failure, brain ischemia, and myocardial infarction. In toxicology studies in dogs and rats, F573 also demonstrated an excellent safety profile.

Indication

Acute liver failure is a life-threatening disease, characterized by a sudden, massive death of liver cells. Although there are hundred thousands of liver failure patients annual, there has been no available therapy for acute-on-chronic liver failure except expensive liver transplants.
Apoptosis, or programmed cell death, is a crucial factor in the maintenance of liver health. Viral and autoimmune hepatitis, cholestatic disease, and metabolic disorders are often associated with enhanced hepatocyte apoptosis. Apoptosis also plays a role in transplantation-associated liver damage, both in ischemia/reperfusion injury and graft rejection.

Clinical development

The Company has licensed exclusive Asian rights to develop F573 for liver diseases, especially for acute liver failure and acute-on-chronic liver failure. GNI also has the option to obtain global rights for the drug. Currently, it is being developed for both oral and injection formulation, based on improved manufacturing methods developed by GNI.
A previous U.S. Phase II trial of another pan-caspase inhibitor PF-03491390 demonstrated the beneficial effect of lowering ALT and AST, the two key indicators of liver function. Most notable, the use of pan-caspase inhibitor is safe for up to three months usage. Further clinical studies of this compound have also suggested that caspases inhibitor is safe and well tolerated in acute-on-chronic liver failure patents.
The Company has filed with the CFDA an IND for F573 under the acute liver failure and acute-on-chronic liver failure indications.